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Restrict the search for
nalidixic acid
to a specific field?
Status:
Investigational
Source:
NCT00076492: Phase 2 Interventional Completed Parkinson Disease
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
GPI-1485 belongs to a class of small molecule compounds called neuroimmunophilin ligands. This class of compounds has been shown to repair and regenerate damaged nerves without affecting normal, healthy nerves. GPI-1485 binds to FK-506-binding proteins. Phase 2 studies have been conducted to assess whether GPI-1485 is able to delay or stop disease progression and improve symptoms in patients with Parkinson's disease (PD), and whether GPI-1485 can help preserve erectile function after prostatectomy.
Status:
Investigational
Source:
NCT00389779: Phase 3 Interventional Completed Hypertension
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Darusentan is an orally active, propanoic acid-based endothelin receptor antagonist (ERA) that selectively blocks endothelin-1 (ET-1) binding to the endothelin type-A (ETA) receptor. Darusentan exhibited subnanomolar binding affinity and approximately 1000-fold selectivity for the ETA receptor in binding experiments conducted in vitro under steady-state conditions. Darusentan is orally bioavailable and, when administered to humans, maximum plasma concentrations are observed within 1–2 h post dosing. The mean elimination half-life is relatively long (>15 h), which is consistent with once-daily dosing. Darusentan is primarily glucuronidated by Phase II enzymes in the liver, and the major route of elimination of Darusentan and its metabolites is via the bile. Some glucuronidated metabolites of Darusentan are also excreted in the urine. Darusentan doses up to 300 mg/day were well tolerated and associated with a manageable safety profile in patients with resistant hypertension (RHTN). The most frequently reported adverse events in Ddarusentan-treated subjects were peripheral edema (17%) and headache (11%), which were mostly mild or moderate in severity. Other commonly reported adverse events in the Darusentan treatment group were sinusitis (8%), dizziness (7%), upper respiratory tract infection (5%) and gastroenteritis (5%). In phase III clinical trial the mean reductions in clinic systolic and diastolic blood pressures were 9/5 mm Hg with placebo, 17/10 mm Hg with Darusentan 50 mg, 18/10 mm Hg with Darusentan 100 mg, and 18/11 mm Hg with Darusentan 300 mg. Unfortunately, phase III clinical trial evaluating Darusentan did not achieve its co-primary efficacy endpoints of achieving a change in systolic and diastolic blood pressure after 14 weeks compared to a placebo. Perhaps for this reason, shortly after the top-line results of this study became known, the sponsor announced that Darusentan would not be developed further for resistant hypertension.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Namirotene [CBS-211A] is a retinoic acid analogue which was undergoing phase II trials with Chauvin in France as 0.02% eye drops for corneal ulcer. It was discontinued later. Namirotene is a synthetic analogue of retinoic acid with differentiation inducing and potential antineoplastic activities. Like other retinoic acid agents, namirotene binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells. When it was associated with 1 alpha,25(OH)2D3, CBS-211A strongly potentiated the 1 alpha,25(OH)2D3-induced inhibition of U937 cell proliferation and caused a dramatic increase in their differentiation toward monocytes/macrophages. The co-inducing effect of CBS-211A was restricted to U937 cells. Our data suggest that CBS-211A may have therapeutic implications in the treatment of certain kinds of myelomonocytic leukemia. CBS-211A also provides an interesting tool to understand the mechanisms involved in the differentiation of myelomonocytic cells.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Lobendazole is a metabolite of veterinary drug thiophanate. Lobendazole possesses teratogenic effect.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Pirodavir (R77975) (ethyl 4-[2-(1-[6-methyl-3-pyridazinyl]-4-piperidinyl)ethoxy]benzoate) and its predecessor (R61837) belong to a series of pyridazine analogues developed by the Janssen Research Foundation. Compared to R61837, pirodavir was 500-fold more potent as an antiviral in vitro, inhibiting 80% of 100 rhinovirus serotypes tested at concentration of 0.064 mg/mL or less. Pirodavir acts at an early stage of the viral replication cycle (up to 40 min after infection) and reduces the yield of selected rhinoviruses 1,000- to 100,000-fold in a single round of replication. The mode of action appears to be serotype specific, since pirodavir was able to inhibit the adsorption of human rhinovirus 9 but not that of human rhinovirus 1A. Pirodavir is a novel capsid-binding antipicornavirus agent with potent in vitro activity against both group A and group B rhinovirus serotypes.
Class (Stereo):
CHEMICAL (ACHIRAL)
Stirimazole is an imidazole derivative patented by Lilly Industries Ltd. as an antiparasitic agent effective against Trypanosoma congolense, T. gambiense, T. rhodesiense, and T. cruzi. Stirimazole inhibited Trichomonas vaginalis in vitro at 0.225 μg/ml and eliminated infected lesions in mice at 20 mg/kg orally. Stirimazole eliminated intestinal amebiasis in rats at 50 mg/kg orally and hepatic amebiasis in hamsters at 100 mg/kg i.p. Stirimazole was curative against Trypanosoma rhodesiense, Trypanosoma cruzi, Trypanosoma gambiense, and Trypanosoma congolense in mice at 25, 100, 12.5, and 25 mg/kg (4 times, i.p.), respectively, and against Trypanosoma vivax in calves at 25 mg/kg i.v.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Phthalylsulfamethizole is the sulfonamide. It was used as an antibacterial agent.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Libenzapril is a long-acting, small polar angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Libenzapril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Libenzapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. Both libenzapril and water transport was found to be significantly higher (about two- to five-fold) in six of the seven different brain regions in hypertensive rats as compared to the normotensive controls.
Status:
Investigational
Source:
NCT00683436: Phase 2 Interventional Terminated Primary Insomnia
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Adipiplon is an oral, partial agonist of the GABAA alpha-3 (α3) receptor that was being developed by Neurogen Corporation for the treatment of insomnia, anxiety disorders and schizophrenia. Adipiplon has been tested in Phase 1 and 2 studies in over 600 subjects for the treatment of insomnia, demonstrating statistical significance compared to placebo on primary endpoints for sleep initiation and maintenance in patients with chronic insomnia. Adipiplon has also demonstrated statistical significance compared to placebo for self-reported quality of sleep in all completed Phase 2 studies to date. Additionally, in studies completed to date it has been well tolerated at all doses tested. Development of adipiplon was discontinued during 2008.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Zoniporide hydrochloride is a novel, potent and selective NHE-1 inhibitor (IC50 = 14 nM). Reduces infarct size in the isolated heart (EC50 = 0.25 nM). Attenuates post-ischemic cardiac contractile dysfunction and ischemia-reperfusion-induced ventricular fibrillation in vivo. Zoniporide hydrochloride represents a novel class of potent and selective human NHE-1 inhibitors with potential utility for providing cardioprotection in a clinical setting.
